1. Field of the Invention
This invention relates to antipicornaviral compounds and their uses.
2. Summary of the Invention
We have found that compounds of Formula I are effective antipicornaviral agents. Accordingly, the present invention relates to compounds of the formula; ##STR2## wherein,
Het.sub.1 is chosen from the group consisting of furyl, oxazolyl, isoxazolyl, oxadiazolyl, tetrazolyl, thiadiazolyl, pyridyl, pyrimidyl, pyridazyl, pyrazyl or any of these substituted with alkyl, alkoxy, hydroxy, cycloalkyl, hydroxyalkyl, hydroxyhaloalkyl, alkoxyalkyl, hydroxyalkoxy, alkyl thioalkyl, alkanoyl alkanoyloxy, alkylsulfinyl alkyl, alkylsulfonylalkyl amino alkyl, alkylaminoalkyl, dialkylaminoalkyl, alkoxycarbonyl, carboxy cyanomethyl, fluoroalkyl or halo.
Y is an alkylene bridge of 3 to 9 carbon atoms.
Het.sub.2 is quinolyl, benzofuranyl, indolyl, benothiazolyl or benzoxazolyl; or these substituted by R.sub.1 and R.sub.2.
R.sub.1 and R.sub.2 are each individually chosen from hydrogen, halo, alkyl, alkenyl, amino, alkylthio, hydroxy, hydroxyalkyl, alkoxyalkyl, alkylthioalkyl, alkylsulfinyl alkyl, alkylsulfonylalkyl, alkoxy, nitro, carboxy, alkoxycarbonyl, dialkylaminoalkyl, alkylaminoalkyl, aminoalkyl, difluoromethyl, trifluoromethyl or cyano;
R.sub.3 is alkoxycarbonyl, alkyltetrazolyl, phenyl or heterocyclyl chosen from benzoxazolyl, benzathiazolyl, thiadiazolyl, imidazolyl, dihydroimidazolyl, oxazolyl, thiazolyl, oxadiazolyl, pyrazolyl, isoxazolyl, isothiazolyl, furyl, triazolyl, tetrazolyl, thiophenyl, pyridyl, pyrimidinyl, pyrazinyl, pyridazinyl or any of the above substituted with alkyl, halo, alkoxyalkyl, cycloalkyl, haloalkyl, hydroxyalkyl, alkoxy, hydroxy, furyl, or thienyl or fluoroalkyl the N-oxide thereof or a pharmaceutically acceptable acid addition salt thereof.
The invention also relates to compositions for combating picornaviruses comprising an antipicornavirally effective amount of a compound of Formula I with a suitable carrier or diluent, and to methods of combating plcornaviruses therewith, including the systemic treatment of picornaviral infections in a mammalian host.